NFkappaB诱饵寡核苷酸。

Daniela De Stefano, Giuseppe De Rosa, Rosa Carnuccio
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引用次数: 0

摘要

分子疗法正在成为治疗炎症性疾病的一种潜在策略。NFkappaB是一种诱导性转录因子,在几种炎症/免疫疾病中起着关键作用,针对NFkappaB的诱饵寡核苷酸(ONs)可以特异性阻断该转录因子的转录活性。这种诱骗细胞的治疗潜力已经在几种慢性炎症性疾病中进行了研究。然而,临床使用的诱饵离子受到几个问题的严重阻碍,包括生物利用度低、半衰期短和细胞内摄取有限。为了克服这些限制,已经研究了对氮化碳进行化学改性和使用递送系统。本文综述了针对NFkappaB的诱骗蛋白在不同疾病的临床前和临床应用方面最有意义的研究,并重点介绍了克服与引诱蛋白相关的药代动力学问题的成功策略。
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NFkappaB decoy oligonucleotides.

Molecular therapy is emerging as a potential strategy for the treatment of inflammatory diseases. Decoy oligonucleotides (ONs) against NFkappaB, an inducible transcription factor that plays a critical role in several inflammatory/immune diseases, can specifically block the transcriptional activity of this transcription factor. The therapeutic potential of such decoy ONs has been investigated in several chronic inflammatory-based diseases. However, the clinical use of decoy ONs is strongly hampered by several issues, including low bioavailability, a short half-life and limited intracellular uptake. Both chemical modifications to ONs and the use of delivery systems have been investigated in order to overcome these limitations. This review summarizes the most meaningful studies on the preclinical and clinical application of decoy ONs against NFkappaB in different diseases, and highlights successful strategies that have overcome the pharmacokinetic issues associated with ONs.

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Current Opinion in Molecular Therapeutics
Current Opinion in Molecular Therapeutics 医学-生物工程与应用微生物
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